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Cautions

Contraindications

• Known or suspected pregnancy.
• Concomitant therapy with potent CYP3A4 inhibitors. (See Interactions.)
• Peripheral vascular disease, CHD, or hypertension.
• Impaired hepatic or renal function.
• Sepsis.
• Known hypersensitivity to ergot alkaloids or any ingredient in the formulation.

Warnings/Precautions

Warnings

Fibrosis

Possible retroperitoneal and pleuropulmonary fibrosis.

Possible fibrotic thickening of the aortic, mitral, tricuspid, and/or pulmonary valves with continuous, long-term administration; do not administer on a chronic daily basis.

Examine patients regularly for development of fibrotic complications; perform appropriate tests (e.g., ECG, laboratory tests, radiographic examination) if signs or symptoms of these conditions occur.

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; fetal growth retardation observed in animals.

General Precautions

Ergotism

Potential for ergotism, manifested by intense arterial vasoconstriction, producing signs and symptoms of peripheral vascular ischemia; if left untreated, can progress to gangrene. Do not exceed recommended dosages.

If signs and symptoms of impaired circulation occur, discontinue therapy and keep affected extremities warm.

Misuse and Abuse

Solitary rectal or anal ulcer associated with abuse of ergotamine suppositories (e.g., use of higher than recommended dosages or continual use at the recommended dose for many years); usually resolves 4–8 weeks following discontinuance of the drug.

Possible withdrawal symptoms (e.g., rebound headache) upon discontinuance of the drug following indiscriminate use over long periods of time.

Fixed-Combination Preparations

Consider the cautions, precautions, and contraindications associated with other drug(s) in fixed-combination preparations.

Specific Populations

Pregnancy

Category X. (See Fetal/Neonatal Morbidity and Mortality and also see Contraindications under Cautions.)

Oxytocic effects are maximal in 3rd trimester; contraindicated in labor and delivery.

Lactation

Distributed into milk; may cause vomiting, diarrhea, weak pulse, seizures, and unstable BP in nursing infants. Discontinue nursing or the drug.

Inhibits prolactin, but no reports of decreased lactation.

Pediatric Use

Safety and efficacy not established in children.

Hepatic Impairment

Use contraindicated.

Renal Impairment

Use contraindicated.

Common Adverse Effects

With oral tablets, numbness and tingling of the fingers and toes, muscle pains in the extremities, weakness in the legs, precordial distress and pain, transient tachycardia or bradycardia, nausea, vomiting, localized edema, itching.

With sublingual tablets, ischemia, cyanosis, absence of pulse, cold extremities, gangrene, precordial distress and pain, ECG changes, muscle pains, transient tachycardia or bradycardia, hypertension, nausea, vomiting, paresthesias, numbness, weakness, vertigo, localized edema, itching.

With rectal suppositories, ischemia, cyanosis, absence of pulse, cold extremities, gangrene, precordial distress and pain, ECG changes, muscle pains.

Drug Interactions

Extensively metabolized, principally by CYP3A4. Inhibits CYP3A.

Drugs Affecting Hepatic Microsomal Enzymes

Potent CYP3A4 inhibitors: Potential pharmacokinetic interaction (increased serum ergotamine concentrations); potentially fatal cerebral ischemia and/or ischemia of the extremities possible. Concomitant use with potent CYP3A4 inhibitors contraindicated.

Less-potent CYP3A4 inhibitors: Similar effects not reported to date; however, consider possibility of serious toxicity during concomitant use.

Specific Drugs